Therapeutically effective calcium diorotate

ABSTRACT

The novel therapeutically valuable compound calcium diorotate, of the structural formula   AND THERAPEUTIC COMPOSITIONS CONTAINING CALCIUM DIOROTATE.

United States Patent Inventor Hans Alfred Nleper 21, 3 Hanover, GermanyAppl. No. 775,539 Filed Nov. 13, 1968 Patented Nov. 16, 1971 PriorityNov. 15, 1967 Great Britain 52,034/67 THERAPEUTICALLY EFFECTIVE CALCIUMDIOROTATE 1 Claim, No Drawings US. Cl 260/256.4, 260/260, 424/25 1 Int.Cl C071! 51/30 Field of Search 260/260, 256.4 C

References Cited UNITED STATES PATENTS 5/1960 Scriabine 260/260Assistant Examiner-R. J. Gallagher Attorney-Cushman, Darby & CushmanABSTRACT: The novel therapeutically valuable compound.eldmsgprotaggthestme r 92914? H H N NH HN and therapeutic compositionscontaining calcium diorotate.

THERAPEUTICALLY EFFECTIVE CALCIUM DIOROTATE H H N N =0 0:! To

NH H\/ I I COO-Ca-OOC Calcium diorotate is synthetized by treatment ofan aqueous solution of orotic acid with a soluble calcium salt in anaqueous solution in stoichiometric amount. The calcium salt, such asCaCl or (CH COO) Ca is added slowly with stirring, and calcium diorotateprecipitates out, and is filtered. The crystals are washed with hotwater and dried.

A white tasteless crystalline powder, is formed. The compound issparingly soluble in the usual solvents, (i.e., less than 0.25 percentsoluble) and the melting point is above 350 C.

According to a further feature of the invention, there are provided newtherapeutic compositions which comprises a therapeutic agent asaforesaid, together with a therapeutically acceptable diluent orextender.

Said compositions are suitable for various uses as follows:

a. Tablets, uncoated, scored or not, or enten'coated (gastric juiceresistant) containing from 0.100 to 0.5 g. of the therapeutic agent. Asuitable daily dose is from 0.200 g. to 1 g.

b. Suppositories containing from 0.100 g. to 0.5 g. of the therapeuticagent preferably in a highly resorbable suppository mass. A suitabledaily dose is 0.200 g. to 1 g.

c. Sterile aqueous solutions in vials (preferably 10 ml.), forintravenous and/or intramuscular injections, containing 10 percent byweight of the therapeutic agent. A suitable daily dose is l to 2 g.

d. Compositions for application to the skin or to mucous membranes,containing from 0.5 to 5 percent by weight of therapeutic agent, such asointment bases or lotion in aqueous resorbable solution, emulsion orsuspension.

e. Ophthalmic preparations such as collyrium containing 0.1 to 2 percentby weight of the therapeutic agent, in an isotonic buffered aqueoussolution.

The compound under its various dosage forms has been found to be activein the treatment of:

l. Overweight 2. Skin diseases such as: psoriasis 3. Inflammatorydiseases such as:

a. arteritis b. thrombophlebitis c. retinitis (1. chronic hepatitis 3.cholitis mucosa 4. Arteriosclerosis 5. Atherosclerosis 6. Autoimmunediseases a. multiple sclerosis b. disseminated encephalitis 7.Inflammatory and osteoporotic decalcification.

I claim as my invention:

1. The compound calcium diorotate, having the structural formula:

